Lipase-catalyzed kinetic resolution of 7-, 8- and 12-membered alicyclic β-amino esters and N-hydroxymethyl-β-lactam enantiomers
摘要:
Enzymatic kinetic resolutions of methyl cis-2-aminocycloheptane-, 2-aminocyclooctane- and 2-aminocyclododecanecarboxylates with Candida antarctica lipase A in diisopropyl ether (E > 200) and of the corresponding N-hydroxymethyl-beta-lactams with Pseudomonas cepacia lipase in dry acetone (E from 27 to > 200) has been performed with 2,2,2-trifluoroethyl butanoate as the best acyl donor, with both enantiomers being obtained. trans-13-Hydroxymethyl-13-azabicyclo[10.2.0]tetradecan-14-one was resolved with vinyl butanoate and Candida antarctica lipase B (E=26) in acetone. (C) 2003 Elsevier Ltd. All rights reserved.
The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
Provided herein are peptides and peptide analogs and methods of treating a metabolic disease, e.g., obesity, diabetes, methods of treating cancer, methods of treating a liver disease, and methods of modulating fatty acid metabolism.
Peptide inhibitors of transcription factor aggregation
申请人:ADRX, INC.
公开号:US11117930B2
公开(公告)日:2021-09-14
This invention relates to materials, such as peptides, and methods to inhibit the aggregation transcription factors, for example p53 inhibitors, p63 inhibitors and p73 inhibitors. More specifically, the invention relates to cancer chemotherapeutics. More specifically, the invention provides pharmaceutical compositions and methods of treating cancer with certain peptides.
Lipase-Catalyzed Enantioselective Ring Opening of Unactivated Alicyclic-Fused β-Lactams in an Organic Solvent
作者:Eniko Forró、Ferenc Fülöp
DOI:10.1021/ol034096o
日期:2003.4.1
A highly efficient and very simple method was developed for the synthesis of enantiopure beta-amino acids (e.g. cispentacin) and beta-lactams through the enzyme-catalyzed enantioselective ring opening of unactivated alicyclic, beta-lactams in organic media. High enantioselectivity (E > 200) was observed when the Lipolase flipase B from Candida antarctica)-catalyzed reactions were performed with H2O (1 equiv) in dilsopropyl ether at 60 degreesC. The resolved products, obtained in good chemical yield (36-47%), could be easily separated.